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Items: 1 to 50 of 133

1.

Further studies on bis-charged tetraazacyclophanes as potent inhibitors of small conductance Ca(2+)-activated K+ channels.

Yang D, Arifhodzic L, Ganellin CR, Jenkinson DH.

Eur J Med Chem. 2013 May;63:907-23. doi: 10.1016/j.ejmech.2013.02.029. Epub 2013 Mar 6.

PMID:
23685886
2.

The slow afterhyperpolarization: a target of β1-adrenergic signaling in hippocampus-dependent memory retrieval.

Zhang L, Ouyang M, Ganellin CR, Thomas SA.

J Neurosci. 2013 Mar 13;33(11):5006-16. doi: 10.1523/JNEUROSCI.3834-12.2013.

3.

Personal reflections on Sir James Black (1924-2010) and histamine.

Ganellin CR.

Inflamm Res. 2011 Jan;60(1):103-10. doi: 10.1007/s00011-010-0269-2. Epub 2010 Oct 27.

PMID:
20978923
4.

The pharmacology of cimetidine, a new histamine H2-receptor antagonist. 1975.

Brimblecombe RW, Duncan WA, Durant GJ, Ganellin CR, Parsons ME, Black JW.

Br J Pharmacol. 2010 Jul;160 Suppl 1:S52-3. doi: 10.1111/j.1476-5381.2010.00854.x. No abstract available.

5.

Refined docking as a valuable tool for lead optimization: application to histamine H3 receptor antagonists.

Levoin N, Calmels T, Poupardin-Olivier O, Labeeuw O, Danvy D, Robert P, Berrebi-Bertrand I, Ganellin CR, Schunack W, Stark H, Capet M.

Arch Pharm (Weinheim). 2008 Oct;341(10):610-23. doi: 10.1002/ardp.200800042.

PMID:
18816585
6.

Molecular features of the prazosin molecule required for activation of Transport-P.

da Silva JF, Walters M, Al-Damluji S, Ganellin CR.

Bioorg Med Chem. 2008 Aug 1;16(15):7254-63. doi: 10.1016/j.bmc.2008.06.037. Epub 2008 Jun 25.

PMID:
18625562
7.

Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR).

Das BC, Madhukumar AV, Anguiano J, Kim S, Sinz M, Zvyaga TA, Power EC, Ganellin CR, Mani S.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):3974-7. doi: 10.1016/j.bmcl.2008.06.018. Epub 2008 Jun 10.

PMID:
18583127
8.

Synthesis and pharmacological testing of polyaminoquinolines as blockers of the apamin-sensitive Ca2+-activated K+ channel (SK(Ca)).

Fletcher DI, Ganellin CR, Piergentili A, Dunn PM, Jenkinson DH.

Bioorg Med Chem. 2007 Aug 15;15(16):5457-79. Epub 2007 May 26.

PMID:
17560109
9.

BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology.

Ligneau X, Perrin D, Landais L, Camelin JC, Calmels TP, Berrebi-Bertrand I, Lecomte JM, Parmentier R, Anaclet C, Lin JS, Bertaina-Anglade V, la Rochelle CD, d'Aniello F, Rouleau A, Gbahou F, Arrang JM, Ganellin CR, Stark H, Schunack W, Schwartz JC.

J Pharmacol Exp Ther. 2007 Jan;320(1):365-75. Epub 2006 Sep 27.

PMID:
17005916
10.

Enhancement of hippocampal pyramidal cell excitability by the novel selective slow-afterhyperpolarization channel blocker 3-(triphenylmethylaminomethyl)pyridine (UCL2077).

Shah MM, Javadzadeh-Tabatabaie M, Benton DC, Ganellin CR, Haylett DG.

Mol Pharmacol. 2006 Nov;70(5):1494-502. Epub 2006 Jul 28.

11.

Histamine and its receptors.

Parsons ME, Ganellin CR.

Br J Pharmacol. 2006 Jan;147 Suppl 1:S127-35.

12.

Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BK(Ca)).

Power EC, Ganellin CR, Benton DC.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):887-90. Epub 2005 Dec 15.

PMID:
16359866
13.

Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach to designing exopeptidase inhibitors.

Ganellin CR, Bishop PB, Bambal RB, Chan SM, Leblond B, Moore AN, Zhao L, Bourgeat P, Rose C, Vargas F, Schwartz JC.

J Med Chem. 2005 Nov 17;48(23):7333-42.

PMID:
16279793
14.

Search for the pharmacophore in prazosin for Transport-P.

Zunszain PA, Federico C, Sechi M, Al-Damluji S, Ganellin CR.

Bioorg Med Chem. 2005 Jun 1;13(11):3681-9.

PMID:
15862997
15.

Search for histamine H3 receptor antagonists with combined inhibitory potency at Ntau-methyltransferase: ether derivatives.

Apelt J, Grassmann S, Ligneau X, Pertz HH, Ganellin CR, Arrang JM, Schwartz JC, Schunack W, Stark H.

Pharmazie. 2005 Feb;60(2):97-106.

PMID:
15739896
16.

Search for histamine H(3) receptor ligands with combined inhibitory potency at histamine N-methyltransferase: omega-piperidinoalkanamine derivatives.

Grassmann S, Apelt J, Ligneau X, Pertz HH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.

Arch Pharm (Weinheim). 2004 Oct;337(10):533-45.

PMID:
15476285
17.

Bis-quinolinium cyclophanes: toward a pharmacophore model for the blockade of apamin-sensitive SKCa channels in sympathetic neurons.

Galanakis D, Ganellin CR, Chen JQ, Gunasekera D, Dunn PM.

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4231-5.

PMID:
15261276
19.

Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain.

Pelloux-Léon N, Fkyerat A, Piripitsi A, Tertiuk W, Schunack W, Stark H, Garbarg M, Ligneau X, Arrang JM, Schwartz JC, Ganellin CR.

J Med Chem. 2004 Jun 3;47(12):3264-74.

PMID:
15163206
20.

4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.

Meier G, Krause M, Hüls A, Ligneau X, Pertz HH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.

J Med Chem. 2004 May 6;47(10):2678-87.

PMID:
15115409
21.

Structural variations of 1-(4-(phenoxymethyl)benzyl)piperidines as nonimidazole histamine H3 receptor antagonists.

Mikó T, Ligneau X, Pertz HH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.

Bioorg Med Chem. 2004 May 15;12(10):2727-36.

PMID:
15110854
22.
23.
24.

Inhibition of the antigen-induced activation of RBL-2H3 cells by cetiedil and some of its analogues.

Narenjkar J, Assem el-SK, Ganellin CR.

Eur J Pharmacol. 2004 Jan 12;483(2-3):107-16.

PMID:
14729097
26.

Protean agonism at histamine H3 receptors in vitro and in vivo.

Gbahou F, Rouleau A, Morisset S, Parmentier R, Crochet S, Lin JS, Ligneau X, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Schwartz JC, Arrang JM.

Proc Natl Acad Sci U S A. 2003 Sep 16;100(19):11086-91. Epub 2003 Sep 5.

27.

Therapeutic implications of constitutive activity of receptors: the example of the histamine H3 receptor.

Schwartz JC, Morisset S, Rouleau A, Ligneau X, Gbahou F, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Arrang JM.

J Neural Transm Suppl. 2003;(64):1-16. Review.

PMID:
12830926
28.

Imidazole derivatives as a novel class of hybrid compounds with inhibitory histamine N-methyltransferase potencies and histamine hH3 receptor affinities.

Grassmann S, Apelt J, Sippl W, Ligneau X, Pertz HH, Zhao YH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.

Bioorg Med Chem. 2003 May 15;11(10):2163-74.

PMID:
12713826
29.

Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.

Mikó T, Ligneau X, Pertz HH, Ganellin CR, Arrang JM, Schwartz JC, Schunack W, Stark H.

J Med Chem. 2003 Apr 10;46(8):1523-30.

PMID:
12672253
30.

Influence of bulky substituents on histamine h(3) receptor agonist/antagonist properties.

Sasse A, Ligneau X, Rouleau A, Elz S, Ganellin CR, Arrang JM, Schwartz JC, Schunack W, Stark H.

J Med Chem. 2002 Aug 29;45(18):4000-10.

PMID:
12190321
31.

Tritylamino aromatic heterocycles and related carbinols as blockers of ca 2+-activated potassium ion channels underlying neuronal hyperpolarization.

Zunszain PA, Shah MM, Miscony Z, Javadzadeh-Tabatabaie M, Haylett DG, Ganellin CR.

Arch Pharm (Weinheim). 2002 Apr;335(4):159-66.

PMID:
12112036
32.

Piperidino-hydrocarbon compounds as novel non-imidazole histamine H(3)-receptor antagonists.

Meier G, Ligneau X, Pertz HH, Ganellin CR, Schwartz JC, Schunack W, Stark H.

Bioorg Med Chem. 2002 Aug;10(8):2535-42.

PMID:
12057642
33.

Progress in the proxifan class: heterocyclic congeners as novel potent and selective histamine H(3)-receptor antagonists.

Grassmann S, Sadek B, Ligneau X, Elz S, Ganellin CR, Arrang JM, Schwartz JC, Stark H, Schunack W.

Eur J Pharm Sci. 2002 May;15(4):367-78.

PMID:
11988398
34.

Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.

Apelt J, Ligneau X, Pertz HH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.

J Med Chem. 2002 Feb 28;45(5):1128-41.

PMID:
11855993
35.

Importance of the lipophilic group in carbamates having histamine H3-receptor antagonist activity.

Kieć-Kononowicz K, Wiecek M, Sasse A, Ligneau X, Elz S, Ganellin CR, Schwartz JC, Stark H, Schunack W.

Pharmazie. 2000 May;55(5):349-55.

PMID:
11828613
36.

The histamine H3 receptor and its ligands.

Stark H, Arrang JM, Ligneau X, Garbarg M, Ganellin CR, Schwartz JC, Schunack W.

Prog Med Chem. 2001;38:279-308. Review. No abstract available.

PMID:
11774797
37.

Synthesis and structure-activity relationships of cetiedil analogues as blockers of the Ca(2+)-activated K+ permeability of erythrocytes.

Roxburgh CJ, Ganellin CR, Athmani S, Bisi A, Quaglia W, Benton DC, Shiner MA, Malik-Hall M, Haylett DG, Jenkinson DH.

J Med Chem. 2001 Sep 27;44(20):3244-53.

PMID:
11563923
38.

Influence of imidazole replacement in different structural classes of histamine H(3)-receptor antagonists.

Meier G, Apelt J, Reichert U, Grassmann S, Ligneau X, Elz S, Leurquin F, Ganellin CR, Schwartz JC, Schunack W, Stark H.

Eur J Pharm Sci. 2001 Jun;13(3):249-59.

PMID:
11384847
39.

Different antagonist binding properties of human and rat histamine H3 receptors.

Stark H, Sippl W, Ligneau X, Arrang JM, Ganellin CR, Schwartz JC, Schunack W.

Bioorg Med Chem Lett. 2001 Apr 9;11(7):951-4.

PMID:
11294398
40.

Calcium-activated potassium channels sustain calcium signaling in T lymphocytes. Selective blockers and manipulated channel expression levels.

Fanger CM, Rauer H, Neben AL, Miller MJ, Rauer H, Wulff H, Rosa JC, Ganellin CR, Chandy KG, Cahalan MD.

J Biol Chem. 2001 Apr 13;276(15):12249-56. Epub 2001 Jan 22.

41.

Benzophenone derivatives and related compounds as potent histamine H3-receptor antagonists and potential PET/SPECT ligands.

Sasse A, Ligneau X, Sadek B, Elz S, Pertz HH, Ganellin CR, Arrang JM, Schwartz JC, Schunack W, Stark H.

Arch Pharm (Weinheim). 2001 Feb;334(2):45-52.

PMID:
11268774
42.

Medicinal chemistry in the development of societies. Biodiversity and natural products.

Monge A, Chorghade M, Erhardt PW, Ganellin CR, Koga N, Lindberg P, Perun TJ, Topliss JG, Trivedi BK, Wermuth CG.

Eur J Med Chem. 2000 Dec;35(12):1121-5.

PMID:
11248411
43.

Clotrimazole analogues: effective blockers of the slow afterhyperpolarization in cultured rat hippocampal pyramidal neurones.

Shah MM, Miscony Z, Javadzadeh-Tabatabaie M, Ganellin CR, Haylett DG.

Br J Pharmacol. 2001 Feb;132(4):889-98.

44.

Anesthetic-like interaction of the sleep-inducing lipid oleamide with voltage-gated sodium channels in mammalian brain.

Nicholson RA, Zheng J, Ganellin CR, Verdon B, Lees G.

Anesthesiology. 2001 Jan;94(1):120-8. Erratum in: Anesthesiology 2001 Apr;94(4):723.

PMID:
11135731
45.

High constitutive activity of native H3 receptors regulates histamine neurons in brain.

Morisset S, Rouleau A, Ligneau X, Gbahou F, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Schwartz JC, Arrang JM.

Nature. 2000 Dec 14;408(6814):860-4.

PMID:
11130725
46.

Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.

Ligneau X, Morisset S, Tardivel-Lacombe J, Gbahou F, Ganellin CR, Stark H, Schunack W, Schwartz JC, Arrang JM.

Br J Pharmacol. 2000 Dec;131(7):1247-50.

47.

Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.

Stark H, Ligneau X, Sadek B, Ganellin CR, Arrang JM, Schwartz JC, Schunack W.

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2379-82.

PMID:
11055360
48.

Novel histamine H(3)-receptor antagonists with carbonyl-substituted 4-(3-(phenoxy)propyl)-1H-imidazole structures like ciproxifan and related compounds.

Stark H, Sadek B, Krause M, Hüls A, Ligneau X, Ganellin CR, Arrang JM, Schwartz JC, Schunack W.

J Med Chem. 2000 Oct 19;43(21):3987-94.

PMID:
11052804
49.
50.

New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.

Sasse A, Sadek B, Ligneau X, Elz S, Pertz HH, Luger P, Ganellin CR, Arrang JM, Schwartz JC, Schunack W, Stark H.

J Med Chem. 2000 Aug 24;43(17):3335-43.

PMID:
10966752

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